卤素取代苯基哌嗪盐酸盐合成工艺研究

Study on the Synthesis of Halo-substituted Phenylpiperazine Hydrochloride

卤素取代苯基哌嗪盐酸盐是治疗过敏、抗抑郁及抗高血压等药物的重要中间体,以二乙醇胺为起始原料,经氯代反应、与卤素取代苯胺的亲核取代反应得到了7个卤代苯基哌嗪盐酸盐,其结构经红外光谱、质谱、核磁共振氢谱确认。通过对投料比和反应时间的研究,确定了一条较优的合成路线,该路线中原料易得,反应容易控制,收率较高,为工业化生产奠定了技术基础。

Halo-substituted phenylpiperazine hydrochlorides are important intermediates for the drugs which are used for treatment of allergy,anti-depressant and anti-hypertensive. Seven halogenated phenylpiperazine hydrochlorides were prepared from diethanolamine via a chlorination reaction and a nucleophilic substitution reaction with halo-substituted aniline. The reaction conditions were optimized. All of the compounds were identified by IR,MS and 1H NMR spectra. The results showed that this route is suitable for industrial production with advantages of low cost, mild reaction conditions and high yield.